| Identification | Back Directory | [Name]
GGTI-297 | [CAS]
181045-83-0 | [Synonyms]
GGTI-297
N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE, TFA | [Molecular Formula]
C26H31N3O3S | [MDL Number]
MFCD02683590 | [MOL File]
181045-83-0.mol | [Molecular Weight]
465.61 |
| Hazard Information | Back Directory | [Description]
GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase). | [Uses]
GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras[1][2]. | [Definition]
ChEBI: (2S)-2-[[[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)phenyl]-oxomethyl]amino]-4-methylpentanoic acid is a leucine derivative. | [in vivo]
GGTI-297 (70 mg/kg; ip; once a day; for 5-7 weeks) inhibits the growth in nude mice of A-549 and Calu-1 xenografts, both of which express K-Ras mutations[2].
| Animal Model: | Nude mice injected (8 week old) with A-549 or Calu-1 cells[2] | | Dosage: | 70 mg/kg | | Administration: | ip; once a day; for 5 weeks (A-549 cells) and 12 weeks (Calu-1) | | Result: | Inhibited the growth in nude mice of A-549 and Calu-1 xenografts.
|
| [References]
[1] Y Qian, et al. Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. Bioorg Med Chem. 1998 Mar;6(3):293-9. DOI:10.1016/s0968-0896(97)10040-2
[2] J Sun, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-73. DOI:10.1038/sj.onc.1201656 |
|
|